4'-去甲基-4-脱氧鬼臼毒素的前药：合成及其抗肿瘤活性评估
Prodrugs of 4'-demethyl-4-deoxypodophyllotoxin: synthesis and evaluation of the antitumor activity.
作者信息
Kim Yong, You Young-Jae, Nam Nguyen Hai, Ahn Byung-Zun
机构信息
College of Pharmacy, Chungnam National University, Taejon, South Korea.
出版信息
Bioorg Med Chem Lett. 2002 Dec 2;12(23):3435-8. doi: 10.1016/s0960-894x(02)00758-8.
Abstract
A series of prodrugs of 4'-demethyl-4-deoxypodophyllotoxin (DDPT) including carbamates (3-8), a carbonate (9) and water-soluble amino acid derivatives (10-17) were prepared and tested for their antitumor activity. The carbamate 6 (2-hydroxyethylcarbamoyl-DDPT), carbonate 9 (2-chloroethyloxycarbonyl-DDPT), and most of amino acid prodrugs (12-17) showed enhanced antitumor activity.
摘要
制备了一系列4'-去甲基-4-脱氧鬼臼毒素（DDPT）的前药，包括氨基甲酸酯类（3-8）、碳酸酯类（9）和水溶性氨基酸衍生物（10-17），并对其抗肿瘤活性进行了测试。氨基甲酸酯6（2-羟乙基氨基甲酰-DDPT）、碳酸酯9（2-氯乙氧基羰基-DDPT）以及大多数氨基酸前药（12-17）显示出增强的抗肿瘤活性。
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